Methanol → 4-chloro-6-[(2S)-2,4-dimethyl-1-piperazinyl]-5-fluoro-2-methylpyrimidine

Participants

Reaction Steps

To 4,6-dichloro-5-fluoro-2-methylpyrimidine (0.309 g, 1.71 mmol) and triethylamine (0.83 mL, 5.98 mmol) in THF (6.0 mL) was added (3S)-1,3-dimethylpiperazine dihydrochloride (Example 64) (0.320 g, 1.71 mmol). MeOH (3 mL) was added to improve solubility and the reaction was stirred for 4 days at room temperature. The solvent was removed in vacuo, and ether, THF and water were added to the resulting residue. The organics were dried (Na2SO4) and concentrated in vacuo to provide 4-chloro-6-[(2S)-2,4-dimethyl-1-piperazinyl]-5-fluoro-2-methylpyrimidine as an orange solid (0.277 g, 63%). LCMS: (M+H)+=259.3.

Provenance & Evidence